Menin-MLL inhibitor MI-2

SKU: orb1305219

Description

MI-2 (MI2) is a small molecule inhibitor that potently disrupts the menin-MLL protein interaction with an IC50 of 446 nM. It is a valuable research tool for studying MLL-rearranged leukemias in both cellular and animal models, aiding in the exploration of targeted therapeutic strategies.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1271738-62-5
• MW: 375.55
• Purity: 97.46%
• Formula: C₁₈H₂₅N₅S₂
• SMILES: CCCc1cc2c(ncnc2s1)N1CCN(CC1)C1=NCC(C)(C)S1
• Target: Epigenetic Reader Domain,Histone Methyltransferase,Apoptosis
• Solubility: Ethanol:70 mg/mL (186.39 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:70 mg/mL (186.39 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.33 mM)

Bioactivity

• Target IC50:
  Menin-MLL:446 nM
• In Vivo:
  MI-2 effectively inhibits cell proliferation and induces apoptosis in human MLL leukemia cell lines bearing various MLL translocations. In HEK293 cells, MI-2 penetrates its protein target, efficiently inhibiting the interaction between menin and MLL-AF9. By downregulating the expression of target genes essential for the oncogenic activity of MLL fusion proteins, MI-2 effectively blocks leukemia transformation mediated by MLL fusion proteins.
• Cell Research:
  The MLL-AF9 and E2A-HLF transduced murine BMC are plated in 12-well plates at the concentration of 5×103 cells/mL with 1 mL methylcellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds. 6 days later colonies are stained with 100 μL iodonitrotetrazolium chloride at final concentration of 1 mg/mL, incubated at 37°C for 30 min and counted. To replate for the 2nd round, colonies are counted at day 6 without staining and cells were washed out by 1×PBS buffer and resuspended in IMDM medium containing 15% FBS, 1% penicillin/streptomycin and IL-3. 5×103 cells are plated in 12-well plates with 1ml methycellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds. 6 days later colonies are stained and counted.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Menin MLL inhibitor MI 2, Menin-MLL, MeninMLL inhibitor MI2, Menin-MLL inhibitor MI-2, MI2, MI-2, MI 2, Menin-MLL Inhibitor, Menin-MLL inhibitor 2, Histone Methyltransferase, HistoneMethyltransferase, EpigeneticReaderDomain, Epigenetic Reader Domain

Compound Identifiers

PubChem CID

54765302